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Aqueous Solubility Determination

Poor aqueous solubility can limit the ability to develop lead compounds as in vivo probes and therapeutics. Aqueous solubility affects absorption, formulation and ability of a compound to be delivered in sufficient concentrations to be active, and even in vitro activity.

The Core offers two types of assays:

Thermodynamic (or Equilibrium) Solubility

Measures solubility of a compound as a saturated solution in equilibrium. Solubility can be dependent on pH and the pKa of the compound.

Typical Assay Conditions:

  • Aqueous buffer: dH20 or buffered solution
  • Incubation: 24 hours at room temperature
  • Analysis: LC-MS/MS after centrifugation
  • Compound Requirements: 2 times 1 mg for each assay condition plus 1 mg for preparation of standards. Please provide material in crystalline form.

Kinetic Solubility

Measures solubility of a compound when added from an existing stock solution in DMSO.

Typical Assay Conditions:

  • Aqueous buffer: dH20 + 0.1-2% DMSO
  • Incubation: Up to 24 hours
  • Analysis: LC-MS/MS after centrifugation
  • Compound Requirements: 10 mM DMSO stock solution
pH dependent solubility graph